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SB431542
| Product Name | SB431542 |
| Price: | Inquiry |
| Catalog No.: | CN00536 |
| CAS No.: | 301836-41-9 |
| Molecular Formula: | C22H16N4O3 |
| Molecular Weight: | 384.39 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | NC(=O)c1ccc(cc1)c1[nH]c(c(n1)c1ccc2c(c1)OCO2)c1ccccn1 |
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| Description | SB-431542 is a potent and selective inhibitor of ALK5 with an IC50 value of 94 nM, and is also an inhibitor of TGF-β Receptor. |
| Target | IC50: 94 nM (ALK5)[2] |
| In Vitro | SB-431542 (1 μM) significantly reduces the TGF-β-induced nuclear accumulation of Smad proteins in A498 cells. SB-431542 inhibits TGF-β1-induced collagen Iα1 and PAI-1 mRNA with IC50 values of 60 and 50 nM, respectively. In addition, SB-431542 inhibits TGF-β1-induced fibronectin mRNA and protein with IC50 values of 62 and 22 nM, respectively[1]. SB-431542 (10 μM) is a selective inhibitor of endogenous activin and TGF-β signaling but has no effect on BMP signaling in NIH 3T3 cells[2]. TRKI, SB-431542, inhibits TGF-beta-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 attenuates the tumor-promoting effects of TGF-beta, including TGF-beta-induced EMT, cell motility, migration and invasion, and vascular endothelial growth factor secretion in human cancer cell lines. SB-431542 induces anchorage independent growth of cells that are growth-inhibited by TGF-beta, whereas it reduces colony formation by cells that are growth-promoted by TGF-beta[3]. SB-431542 (0.3 μM) inhibits cell proliferation induced by TGF-β in MG63 cells[4]. |
| In Vivo | SB-431542 (10 mg/kg, i.p.) decreases lung metastasis but does not significantly alter growth of the primary tumor 4T1 xenograft[5]. |
| Cell Assay | A498 cells are seeded at 5,000 to 10,000 cells/well in 96-well plates. The cells are serum-deprived for 24 h and then treated with SB-431542 for 48 h to assess the cellular toxicity. Cell viability is determined by incubating cells for 4 h with XTT labeling and electron coupling reagent according to the manufacturer's directions. Live cells with active mitochondria produce an orange-colored product, formazan, which is detected using a plate reader at between A 450 nm and A 500 nm with a reference wavelength greater than 600 nm. The absorbance values correlate with the number of viable cells. |
| Animal Admin | Ten thousand 4T1 cells are injected subcutaneously into the second mammary fat pad of 6-week-old Balb/c female mice. Tumors are measured twice weekly, and volume is calculated using the following formula: Volume = width2×length×0.52. Mice are randomly assigned to two treatment groups: control, n = 14 (20% DMSO/80% corn oil); SB-431542-treated, n = 15 (10 mg/kg body weight in 20% DMSO/80% corn oil, administered intraperitoneally three times per week starting one day after tumor cell inoculation. Primary tumors are resected when the volume at day 10 post-injection of 4T1 cells. All mice are monitored daily and euthanized after 4 weeks. The metastases are dissected to snap-freeze for further analysis. |
| Density | 1.4±0.1 g/cm3 |
| Boiling Point | 662.4±55.0 °C at 760 mmHg |
| Flash Point | 354.4±31.5 °C |
| Exact Mass | 384.122253 |
| PSA | 103.12000 |
| LogP | 4.28 |
| Vapour Pressure | 0.0±2.0 mmHg at 25°C |
| Storage condition | −20°C |